Bone-seeking therapeutic radiopharmaceuticals

Abstract

Bone-seeking therapeutic radiopharmaceuticals are utilized on the basis of the radionuclide’s particulate emissions (primarily low to intermediate beta emission). The requirements therefore are different from those of bone imaging agents that consist mainly of short-lived single photon emitters. Lately, the therapeutic bone seeking radiopharmaceuticals have attained increasing importance due to their potential role in alleviating pain from osseous metastases in cancer patients, for the treatment of joint pain resulting from inflamed synovium (radiosynoviorthesis, or radiosynovectomy), or from various other forms of arthritic disease. There is, however, a paucity of published data on the bio-pharmacokinetics of these agents when used following intravenous administration for bone pain palliation. This paper will briefly review and summarize the presently available chemical and biopharmacokinetic information on the various clinically approved as well as experimental bone-localizing therapeutic radiopharmaceuticals, and make projections on their clinical application for the treatment of primary/metastatic cancer in bone.<br>Radiofármacos para terapia em nível ósseo são utilizados devido a emissão de radiação particular pelo radionuclídeo (primariamente beta de baixa e média). Portanto, as necessidades são diferentes daquelas usadas para imagem óssea que consiste principalmente de emissores de fótons de meia-vida curta. Ultimamente, a terapia do esqueleto com radiofármaco tem alcançado uma importância crescente devido ao papel em potencia de aliviar a dor de metástases ósseas em pacientes com câncer, para o tratamento de dor nas articulações devido a inflamação sinovial sinovite (radiosinovite ou radiosinovectomia), ou de várias outras formas de doenças articulares. Portanto, existe uma falta de publicações sobre a bio-farmacocinética desses agentes quando administrados intravenosamente como paliativo para dor óssea. Este artigo irá revisar rapidamente e resumir as informações sobre a química e a biofarmacocinética dos vários radiofármacos aprovados clinicamente e em experimentação disponíveis até o presente momento para terapêutica do esqueleto e fazer projeções para o tratamento clínico do câncer primário/metastático no osso

Radiometals for Combined Imaging and Therapy

“…138 Both 89 Sr and 32 P were investigated as early as the 1940s for the treatment of metastatic cancer to bone, 139 and 89 Sr received FDA approval for routine application in 1993. 140 Radiation is of proven benefit for pain palliation, and there is a growing interest in the therapeutic potential of bone-seeking radiopharmaceuticals. Such palliative treatment of patients with advanced metastatic disease of the skeleton can improve their quality of life dramatically and thus is an important application with many advantages over traditional analgesics and external radiation.…”

“…A comparison of 89 Sr-chloride, 153 Sm-EDTMP, 32 P, 188 Re-HEDP, and 117m Sn-DTPA was made by Srivastava. 140 While only limited clinical trials were cited, 117m Sn offers very favorable characteristics. The initial dose is higher than that obtained by 89 Sr, and in vitro and in vivo stabilities are very high.…”

Radiochemical processing of nuclear-reactor-produced radiolanthanides for medical applications

“…Not all radiolanthanides can be used in nuclear medicine. To be considered as appropriate radiopharmaceutical, several criteria have to be met [4,9,40,41]. First of all, the decay characteristics of the radiolanthanide are important, including the type of radiation (e.g.…”

The role of electron-emitting radiopharmaceuticals in the palliative treatment of metastatic bone pain and for radiosynovectomy: applications of conversion electron emitter Tin-117m

“…These articles have provided an outline of the principles for production, and decay considerations for therapeutic radionuclides (Volkert et al, 1991), clarified the relationships between tumor size and curability for therapy with beta-emitting radionuclides (Wheldon, 1994;O'Donoghue et al, 1995), and set the criteria for the selection of radionuclides for cancer radioimmunotherapy . A recent review describes the developments in the application of therapeutic radiopharmaceuticals in preclinical studies, as well as in the clinical setting (Ercan and Caglar, 2000;Srivastava, 2002). Nuclear medicine has indeed experienced a resurgence of interest in radiotherapeutic procedures.…”